Summary The long-term goal of this application is to provide stable research funding for a Cancer Pharmacokinetics Research Specialist within the University of Pittsburgh Cancer Institute (UPCI) Cancer Pharmacokinetics and Pharmacodynamics Facility (CPPF). The activities of the Cancer Pharmacokinetics Research Specialist can be categorized broadly into: (1) Pharmacokinetic assay development and validation; (2) Preclinical pharmacokinetics; and (3) Clinical pharmacokinetics. The Cancer Pharmacokinetics Research Specialist plays an absolutely critical role in developing and validating novel LC-MS/MS methodologies, and applying them to precisely delineate the PK and metabolism of novel and established agents. The stated new research directions of: (1) generic assay platform development; (2) metabolite structural elucidation by high-resolution mass spectrometer; and (3) population-pharmacokinetic analyses of clinical pharmacokinetic data, are relevant and sure to enhance the research output of the CPPF. This award will allow the CPPF Cancer Pharmacokinetics Research Specialist to continue to be at the cutting edge, with the ultimate aim of serving the scientific community in early drug development needs.